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WO2022244765A1 - Goutte oculaire pour supprimer la myopie - Google Patents

Goutte oculaire pour supprimer la myopie Download PDF

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Publication number
WO2022244765A1
WO2022244765A1 PCT/JP2022/020514 JP2022020514W WO2022244765A1 WO 2022244765 A1 WO2022244765 A1 WO 2022244765A1 JP 2022020514 W JP2022020514 W JP 2022020514W WO 2022244765 A1 WO2022244765 A1 WO 2022244765A1
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WO
WIPO (PCT)
Prior art keywords
myopia
eye
suppressing
bunazosin
eye drop
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2022/020514
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English (en)
Japanese (ja)
Inventor
憲煜 丁
俊英 栗原
一男 坪田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tsubota Laboratory Inc
Original Assignee
Tsubota Laboratory Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tsubota Laboratory Inc filed Critical Tsubota Laboratory Inc
Priority to KR1020237038535A priority Critical patent/KR20240008848A/ko
Priority to CA3216748A priority patent/CA3216748A1/fr
Priority to US18/561,634 priority patent/US20240366626A1/en
Priority to CN202280035569.4A priority patent/CN117320726A/zh
Priority to EP22804676.9A priority patent/EP4342472A4/fr
Priority to AU2022276728A priority patent/AU2022276728A1/en
Publication of WO2022244765A1 publication Critical patent/WO2022244765A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia

Definitions

  • the present invention relates to eye drops for suppressing myopia.
  • Myopia is especially common among Asians, especially Japanese, and the percentage of strong myopia of -5D or higher is also high.
  • myopia has been increasing all over the world, and the percentage of children with unaided visual acuity of less than 1.0 is increasing year by year in Japan. It is also known that myopia progresses rapidly during the childhood period from 7 to 12 years old (see Non-Patent Document 1).
  • Myopia is classified into refractive myopia, accommodative myopia (pseudomyopia), and axial myopia according to its onset mechanism, but myopia progression in school children is mainly axial myopia.
  • the human eye is hyperopic immediately after birth, and the extent of hyperopia decreases due to eye axis extension during growth, and becomes emmetropia when children enter school. Axial elongation after this emmetropic phenomenon directly leads to myopia, and the axial length once elongated cannot be restored. Therefore, it is believed that suppression of axial extension during the period from growth to school age is effective for preventing or treating myopia (see Non-Patent Document 2).
  • the ocular axis extends not only in the growth period but also in adults, and it is said that the elongation of the ocular axis in adults is a risk factor for various ocular diseases.
  • a therapeutic agent for preventing myopia has been proposed, for example, a Rho kinase inhibitor (see Patent Document 1), bradykinin (Patent Document 2), crocetin (Patent Document 3), etc. have been proposed.
  • An object of the present invention is to provide a new eye drop for suppressing myopia.
  • the ophthalmic solution for suppressing myopia according to the present invention is characterized by containing bunazosin.
  • the eye drops for suppressing myopia according to the present invention will be explained.
  • the present invention is not limited to the following embodiments and examples, and includes various modifications and applications within the scope of the present invention.
  • Eye drops for suppressing myopia The present inventors focused on the fact that some eye drops for glaucoma are effective in suppressing the progress of myopia, and attempted to find out the effect of suppressing the progress of myopia from existing eye drops for glaucoma.
  • glaucoma eye drops were instilled into a mouse model of myopia, the axial length and refractive index were measured, and whether or not there was an effect of suppressing progression of axial myopia was evaluated.
  • an eye drop containing bunazosin is effective as an eye drop for suppressing myopia.
  • the type of ophthalmic solution containing bunazosin is not particularly limited, it is preferably an aqueous ophthalmic solution.
  • other active ingredients pharmaceutically active ingredients, physiologically active ingredients, other glaucoma eye drop ingredients, etc.
  • the eye drops may contain one or more of them by appropriately selecting various ingredients and additives in accordance with conventional methods, depending on the application and form, within the range that does not impair the effects of the present invention. can be done.
  • these components or additives include various additives such as perfumes or cooling agents, preservatives, bactericides or antibacterial agents, pH adjusters, chelating agents, stabilizers, tonicity agents, and buffers. can be mentioned.
  • the content of bunazosin is set to a realistic amount. It is preferable to use it, and it can be blended within a range that does not impair the effects of the present invention.
  • the usage and dosage of the eye drops vary depending on the patient's symptoms, age, etc., but usually about 1 to 6 times a day, about 1 to 2 drops per time.
  • the present invention uses bunazosin-containing eye drops as myopia-suppressing eye drops.
  • the present invention can be expressed as ii) use of a composition containing bunazosin for the manufacture of an eye drop for myopia reduction, and (ii) a method for reducing myopia by instilling a composition containing bunazosin as an eye drop.
  • the "myopia suppressing effect" referred to in the present application is an effect of suppressing progression of axial myopia.
  • mice C57BL6/J, CLEA Japan, Inc.
  • D is an abbreviation for Diopter, which is the unit of refractive power of the lens
  • Eyes were fitted with 30D lenses to induce myopia.
  • Instillation was continued for 3 weeks, with PBS (Phosphate Buffered Saline) instillation as a control group and bunazosin instillation as a test group.
  • PBS Phosphate Buffered Saline
  • Bunazosin is the main component of detantol ophthalmic solution, and bunazosin was applied using detantol 0.01% ophthalmic solution (manufactured by Santen Pharmaceutical Co., Ltd., 1 mL of which contains 0.1 mg of bunazosin hydrochloride).
  • the frequency of instillation was 2 drops once a day and 2 drops a day (2 drops each in the morning and evening). After 3 weeks, the refractive index and axial length of the mouse eyeball were measured, and the amount of change was calculated.
  • * indicates that p ⁇ 0.05
  • ** indicates that p ⁇ 0.01 (same in the figures of the present application).
  • Refractive values were measured using an infrared photoreflector for mice (Infrared photorefractor for mice, manufactured by Professor Schaeffel, University of Tubingen). Spectral domain optical coherence tomography (Envisu R4310, manufactured by Leica) was used to measure the axial length.
  • FIG. 2 shows the refractive index results. The more negative the refractive index, the more myopic.
  • the eye with the ⁇ 30D lens became myopic, which was significantly different from the eye with the 0D lens.
  • the eye drop group there was no significant difference between the eye with the ⁇ 30D lens and the eye with the 0D lens, and it was found to be effective in suppressing myopia. It should be noted that the effect of suppressing myopia was observed with the one-time instillation rather than the two-time instillation.
  • Figure 3 shows the results of the axial length of the eye. The greater the axial length value, the more myopic.
  • the axial length of the eye with the -30D lens was elongated, and there was a significant difference with the eye with the 0D lens.
  • the instillation group there was almost no difference in axial length between the two eyes, and a myopia-suppressing effect was observed. No difference was observed between the one-time instillation and the two-time instillation.
  • Example 2 Mice similar to Experiment 1 were used and myopia was induced. Eye instillation was continued for 3 weeks, PBS eye instillation was used as a control group, and unoprostone eye instillation was used as a test group. Unoprostone is the main component of Rescula ophthalmic solution. Unoprostone eye drop is Rescula ophthalmic solution 0.12% (Nitto Medic Co., Ltd., 1 mL contains 1.2 mg of isopropyl unoprostone) eye drops (both eyes, once a day). 2 drops each time). After 3 weeks, the refractive index and axial length of the mouse eyeball were measured, and the amount of change was calculated. Refractive index measurement and axial length measurement are the same as in Experiment 1.
  • FIG. 4 shows the refractive index results.
  • the eye with the ⁇ 30D lens became myopic, which was significantly different from the eye with the 0D lens.
  • both eyes became myopic, and no myopia-suppressing effect was observed with instillation.
  • Fig. 5 shows the results of eye axial length.
  • the axial length of the eye with the -30D lens was elongated, and there was a significant difference with the eye with the 0D lens.
  • no significant difference was observed in the axial length of both eyes in the instillation group.

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Rehabilitation Tools (AREA)

Abstract

Le problème décrit par la présente invention est de fournir une nouvelle goutte oculaire pour supprimer la myopie. À cet effet, le problème susmentionné a été résolu en utilisant une goutte oculaire contenant de la bunazosine en tant que goutte oculaire pour supprimer la myopie. La présente goutte oculaire pour supprimer la myopie est efficace pour supprimer la myopie.
PCT/JP2022/020514 2021-05-17 2022-05-17 Goutte oculaire pour supprimer la myopie Ceased WO2022244765A1 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1020237038535A KR20240008848A (ko) 2021-05-17 2022-05-17 근시억제용 점안제
CA3216748A CA3216748A1 (fr) 2021-05-17 2022-05-17 Goutte oculaire pour supprimer la myopie
US18/561,634 US20240366626A1 (en) 2021-05-17 2022-05-17 Ophthalmic preparation for myopia suppression
CN202280035569.4A CN117320726A (zh) 2021-05-17 2022-05-17 抑制近视用滴眼剂
EP22804676.9A EP4342472A4 (fr) 2021-05-17 2022-05-17 Goutte oculaire pour supprimer la myopie
AU2022276728A AU2022276728A1 (en) 2021-05-17 2022-05-17 Eye drop for suppressing myopia

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2021-082858 2021-05-17
JP2021082858A JP6917103B1 (ja) 2021-05-17 2021-05-17 近視抑制用点眼剤

Publications (1)

Publication Number Publication Date
WO2022244765A1 true WO2022244765A1 (fr) 2022-11-24

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Family Applications (1)

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PCT/JP2022/020514 Ceased WO2022244765A1 (fr) 2021-05-17 2022-05-17 Goutte oculaire pour supprimer la myopie

Country Status (9)

Country Link
US (1) US20240366626A1 (fr)
EP (1) EP4342472A4 (fr)
JP (1) JP6917103B1 (fr)
KR (1) KR20240008848A (fr)
CN (1) CN117320726A (fr)
AU (1) AU2022276728A1 (fr)
CA (1) CA3216748A1 (fr)
TW (1) TW202313058A (fr)
WO (1) WO2022244765A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4582103A4 (fr) 2022-08-31 2025-12-03 Tsubota Lab Inc Gouttes oculaires contenant un alpha1-bloquant pour inhiber la progression de la myopie

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63301822A (ja) * 1987-06-01 1988-12-08 Eisai Co Ltd 角膜透過促進点眼剤
JP2003292442A (ja) * 2002-01-29 2003-10-15 Santen Pharmaceut Co Ltd ブナゾシンとプロスタグランジン類からなる緑内障治療剤
WO2006137368A1 (fr) * 2005-06-21 2006-12-28 Kowa Co., Ltd. Agent prophylactique ou remède pour le glaucome
WO2010010702A1 (fr) 2008-07-24 2010-01-28 国立大学法人大阪大学 Agent prophylactique ou thérapeutique pour la myopie axiale
JP2011144111A (ja) 2010-01-12 2011-07-28 Osaka Univ 軸性近視の予防または治療剤
JP2016132616A (ja) * 2015-01-15 2016-07-25 大内新興化学工業株式会社 眼疾患治療用ナノ粒子製剤
WO2018212152A1 (fr) 2017-05-15 2018-11-22 株式会社坪田ラボ Composition et aliment fonctionnel permettant de prévenir la myopie

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003004058A1 (fr) * 2001-07-02 2003-01-16 Santen Pharmaceutical Co., Ltd. Agents de protection du nerf optique contenant un bloqueur de recepteur $g(a)1 en tant qu'ingredient actif
AU2018304450B2 (en) * 2017-07-20 2024-05-16 Seinda Pharmaceutical Guangzhou Corporation Composition and methods for the treatment of myopia
SG11201907400YA (en) * 2018-07-18 2020-02-27 Univ Wenzhou Medical Method for treating myopia and application in preparation of medicament
JP7670945B2 (ja) * 2018-10-26 2025-05-01 オーパス・ジェネティクス・インコーポレイテッド 老眼、散瞳、および他の眼障害の治療のための方法および組成物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63301822A (ja) * 1987-06-01 1988-12-08 Eisai Co Ltd 角膜透過促進点眼剤
JP2003292442A (ja) * 2002-01-29 2003-10-15 Santen Pharmaceut Co Ltd ブナゾシンとプロスタグランジン類からなる緑内障治療剤
WO2006137368A1 (fr) * 2005-06-21 2006-12-28 Kowa Co., Ltd. Agent prophylactique ou remède pour le glaucome
WO2010010702A1 (fr) 2008-07-24 2010-01-28 国立大学法人大阪大学 Agent prophylactique ou thérapeutique pour la myopie axiale
JP2011144111A (ja) 2010-01-12 2011-07-28 Osaka Univ 軸性近視の予防または治療剤
JP2016132616A (ja) * 2015-01-15 2016-07-25 大内新興化学工業株式会社 眼疾患治療用ナノ粒子製剤
WO2018212152A1 (fr) 2017-05-15 2018-11-22 株式会社坪田ラボ Composition et aliment fonctionnel permettant de prévenir la myopie

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
IGAKU NO AYUMI, JOURNAL OF CLINICAL AND EXPERIMENTAL MEDICINE, vol. 253, no. 2, 2015
NITTA, KOJI: "Treatment of pathologic myopia 1. Glaucoma with high myopia", JOURNAL OF THE EYE, MEDICAL AOI PUBLICATION, JP, vol. 37, no. 5, 1 May 2020 (2020-05-01), JP , pages 559 - 574, XP009541131, ISSN: 0910-1810 *
OPHTHALMOLOGY, vol. 58, no. 6, 2016, pages 635 - 641
See also references of EP4342472A4

Also Published As

Publication number Publication date
JP6917103B1 (ja) 2021-08-11
EP4342472A1 (fr) 2024-03-27
TW202313058A (zh) 2023-04-01
JP2022176427A (ja) 2022-11-30
KR20240008848A (ko) 2024-01-19
US20240366626A1 (en) 2024-11-07
CA3216748A1 (fr) 2022-11-24
CN117320726A (zh) 2023-12-29
AU2022276728A1 (en) 2023-11-09
EP4342472A4 (fr) 2024-10-30

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